公开(公告)号：US4697019A

公开(公告)日：1987-09-29

申请号：US824205

申请日：1986-03-21

申请人： Francis D. King

发明人： Francis D. King

IPC分类号： A61K31/435 ,  A61K31/445 ,  A61P1/00 ,  A61P43/00 ,  C07D221/00 ,  C07D223/04 ,  C07D227/00 ,  C07D471/08 ,  C07D487/08 ,  C07D221/04 ,  C07D223/14

CPC分类号： C07D471/08 ,  C07D223/04

摘要： A compound of formula (XXII): ##STR1## or a compound of formula (XXIII): ##STR2## wherein in formula (XXIII), j.sup.1 -1 is 1 to 4; and Q.sub.6 and Q.sub.7 are on the same carbon atom; and wherein, in formulae (XXII) and (XXIII), Q.sub.6 is NH.sub.2 and Q.sub.7 is H, and either p is 0 to 2 and q is 1; or p is 1 and q is 0 to 3; and one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl --C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen; and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl.

摘要翻译： （XXII）化合物：ⅩⅩⅫ或式（ⅩⅩⅢ）化合物：其中在式（ⅩⅩⅢ）中，j1-1为1至4; Q6和Q7位于相同的碳原子上; 并且其中，在式（XXII）和（XXIII）中，Q 6为NH 2且Q 7为H，p为0〜2，q为1。 或p为1，q为0至3; R 5和R 6中的一个是氢，C 1-6烷基，苯基或苯基-C 1-3烷基，该苯基部分可被C 1-6烷基，C 1-6烷氧基，CF 3或卤素取代; R 5和R 6中的另一个是氢或C 1-6烷基。

公开(公告)号：US4678782A

公开(公告)日：1987-07-07

申请号：US679574

申请日：1984-12-07

申请人： Roger J. Ponsford ,  Michael J. Pearson ,  Stephen C. Finch

发明人： Roger J. Ponsford ,  Michael J. Pearson ,  Stephen C. Finch

IPC分类号： C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61K31/425 ,  A61P31/04 ,  C07D205/085 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/10 ,  C07F7/18 ,  C07F9/568 ,  A61K31/495

CPC分类号： C07D403/04 ,  C07D205/085 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/10 ,  C07F9/5683

摘要： A monocyclic .beta.-lactam antibiotic having a formamido substitutent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.

公开(公告)号：US4670431A

公开(公告)日：1987-06-02

申请号：US572195

申请日：1984-01-19

申请人： Peter H. Milner

发明人： Peter H. Milner

IPC分类号： C07D241/08 ,  C07D499/00 ,  C07D499/44 ,  C07D501/20 ,  C07D501/57 ,  A61K31/43 ,  A61K31/545 ,  C07D499/46 ,  C07D501/00 ,  C07D501/18

CPC分类号： C07D241/08 ,  C07D499/00

摘要： A compound having the partial structure (A): ##STR1## wherein n is 1 or 2.

摘要翻译： 具有部分结构（A）的化合物：其中n为1或2。

公开(公告)号：US4647558A

公开(公告)日：1987-03-03

申请号：US459675

申请日：1983-01-20

申请人： Roger J. Ponsford ,  Michael J. Pearson ,  Stephen C. Finch

发明人： Roger J. Ponsford ,  Michael J. Pearson ,  Stephen C. Finch

IPC分类号： C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61K31/425 ,  A61P31/04 ,  C07D205/085 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/10 ,  C07F7/18 ,  C07F9/568 ,  C07D401/12

CPC分类号： C07D403/04 ,  C07D205/085 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07F7/10 ,  C07F9/5683

摘要： A monocyclic .beta.-lactam antibiotic having a formamido substituent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.

摘要翻译： 包括在3S位具有甲酰氨基取代基的单环β-内酰胺抗生素，包括式（I）的化合物：其中R是-SO 3 H; -PO（OH）Y，其中Y为C 1-6烷氧基，羟基，芳氧基，C 1-6烷基或芳基; 其中Z代表C1-6烷基或芳基; 其中Z 1和Z 2可以相同或不同，各自表示氢，C 1-6烷基，芳基，氨基或C 1-6烷氧基，或者Z 1和Z 2一起形成杂环的残基; -OSO3H; 或，其中X是氢或羟基; R1是氨基，保护的氨基或羧基酰基氨基，R2和R3独立地选自氢或1至18个碳原子的烃基。

公开(公告)号：US4645671A

公开(公告)日：1987-02-24

申请号：US754656

申请日：1985-07-15

申请人： John B. Harbridge

发明人： John B. Harbridge

IPC分类号： A61K31/43 ,  C07D257/06 ,  C07D503/00 ,  C07F7/18 ,  A61K35/00 ,  A61K35/66 ,  A61K35/74

CPC分类号： C07D257/06 ,  A61K31/43 ,  C07D503/00 ,  C07F7/1896

摘要： Tetrazolyl derivatives of clavulanic acid are described, having the formula: ##STR1## wherein X is an optionally substituted tetrazolyl group attached via a nitrogen atom. These compounds are useful as antibiotics and .beta.-lactamase inhibitors.

公开(公告)号：US4640928A

公开(公告)日：1987-02-03

申请号：US782508

申请日：1985-10-01

申请人： Kenneth Willcocks

发明人： Kenneth Willcocks

IPC分类号： C07D311/68 ,  C07D405/04 ,  A61K31/35

CPC分类号： C07D405/04 ,  C07D311/68

摘要： Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, benzoyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.3 and R.sub.4 together are C.sub.2-5 polymethylene having anti-hypertensive activity.

摘要翻译： 式（I）的化合物：其中：R 1和R 2中的任一个是氢，另一个选自C 1-6烷基羰基，苯甲酰基，C 1-6烷氧基羰基，C 1-6烷基羰氧基，C 1 -6烷基羟基甲基，硝基，氰基，氯，三氟甲基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基，C 1-6烷氧基亚磺酰基，C 1-6烷氧基磺酰基，C 1-6烷基羰基氨基，C 1-6烷氧基羰基氨基，C 1-6烷基 - 硫代羰基，C 1 -6烷氧基 - 硫代羰基，C 1-6烷基 - 硫代羰基氧基，C 1-6烷基 - 硫醇甲基，甲酰基或氨基亚磺酰基，氨基磺酰基或氨基羰基，氨基部分任选被一个或两个C 1-6烷基或C 1-6烷基亚磺酰氨基取代， C 1-6烷基磺酰氨基C 1-6烷氧基亚磺酰氨基或被C 1-6烷基羰基，硝基或氰基末端取代的C 1-6烷氧基磺酰基氨基或亚乙基，或-C（C 1-6烷基）NOH或-C（C 1-6烷基）NNH 2，或一个 R 1和R 2为硝基，氰基或C 1-3烷基羰基，另一个为任选被一个或两个C取代的甲​​氧基或氨基 1-6烷基或C 2-7烷酰基; R3和R4之一是氢或C1-4烷基，另一个是C1-4烷基，R3和R4一起是具有抗高血压活性的C2-5多亚甲基。

公开(公告)号：US4621089A

公开(公告)日：1986-11-04

申请号：US704621

申请日：1985-02-22

申请人： Robert W. Ward ,  Ian Hughes

发明人： Robert W. Ward ,  Ian Hughes

IPC分类号： A61K31/435 ,  A61P29/00 ,  A61P37/08 ,  C07D231/38 ,  C07D471/04 ,  A61K31/44

CPC分类号： C07D231/38 ,  C07D471/04

摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is NR wherein R is hydrogen or C.sub.1-6 alkyl, oxygen, sulphur, SO or SO.sub.2 ;R.sub.1 is COR.sub.5 wherein R.sub.5 is hydroxy, or COR.sub.5 is a pharmaceutically acceptable ester or amide group; or CF.sub.3 ; and R.sub.2 is hydrogen, C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; or R.sub.2 is COR.sub.5 as defined or CF.sub.3 and R.sub.1 is hydrogen;R.sub.3 is C.sub.1-10 alkyl, optionally substituted by hydroxy, C.sub.1-4 alkoxy, thiol, C.sub.1-4 alkylthio or NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.3-6 polymethylene; C.sub.2-10 alkenyl or phenyl optionally substituted by one or two of halogen, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, hydroxy, nitro, cyano, C.sub.2-10 acyloxy, NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or COR.sub.10 wherein R.sub.10 is hydroxy, C.sub.1-6 alkoxy or NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen or C.sub.1-6 alkyl; andR.sub.4 is hydrogen; or C.sub.1-4 alkyl or benzyl attached at nitrogen atom 1 or 2 having anti-inflammatory and/or anti-allergy activity, a process for their preparation and their use as pharmaceuticals.

摘要翻译： 式（I）化合物及其药学上可接受的盐：其中：X为NR，其中R为氢或C1-6烷基，氧，硫，SO或SO2; R1是COR5，其中R5是羟基，或COR5是药学上可接受的酯或酰胺基; 或CF3; 且R 2为氢，C 1-6烷基或任选被卤素，CF 3，C 1-4烷氧基或C 1-4烷基取代的苯基; 或R2是如所定义的COR5或CF 3，R 1是氢; R 3是任选被羟基，C 1-4烷氧基，硫醇，C 1-4烷硫基或NR 6 R 7取代的C 1-10烷基，其中R 6和R 7独立地是氢或C 1-6烷基或一起是C 3-6 - 多亚甲基; 任选被一个或两个卤素，CF 3，C 1-4烷氧基，C 1-4烷基，羟基，硝基，氰基，C 2-10酰氧基，NR 8 R 9取代的C 2-10烯基或苯基，其中R 8和R 9独立地选自氢，C 1 C6烷基，C2-7烷酰基或C1-6烷基磺酰基或COR10，其中R10是羟基，C1-6烷氧基或NR11R12，其中R11和R12独立地选自氢或C1-6烷基; R4为氢; 或在具有抗炎和/或抗过敏活性的氮原子1或2上连接的C 1-4烷基或苄基，其制备方法及其作为药物的用途。

公开(公告)号：US4612319A

公开(公告)日：1986-09-16

申请号：US484317

申请日：1983-04-12

申请人： Francis D. King

发明人： Francis D. King

IPC分类号： C07D223/04 ,  C07D471/08 ,  A61K31/445 ,  C07D453/00

CPC分类号： C07D471/08 ,  C07D223/04

摘要： A compound of formula (I), or a pharmaceutically acceptable salt, or N-oxide thereof, or a solvate of any of the foregoing: ##STR1## wherein p is 0 to 2; q is 0 to 3; j is 0 to 4;one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl; andA is of formula (II): ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are each independently selected from hydrogen, halogen, CF.sub.3 C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 carboxylic acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene; or any two together are C.sub.1-2 alkylenedioxy;(i) R.sub.1 is independently any one of the values for R.sub.2, R.sub.3 or R.sub.4 except hydrogen or together with R.sub.2 is C.sub.1-2 alkylenedioxy, C.sub.1-2 oxyalkylenethio, C.sub.2-3 alkyleneoxy or N-(C.sub.1-2 oxyalkylene)-N-C.sub.1-6 alkylamino; and one of X and Y is CO and the other is NH; or(ii) X is CO and Y is NR.sub.16 where R.sub.1 and R.sub.16 together areC.sub.1-2 alkylene; the nitrogen atom depicted in formula (I) is separated from the nearest nitrogen atom in the moiety A by at least 2 carbon atoms; a process therefor and compositions thereof.

摘要翻译： 式（I）化合物或其药学上可接受的盐或N-氧化物，或上述任何一种的溶剂合物：其中p为0至2; q为0〜3; j为0〜4; R 5和R 6之一是氢，C 1-6烷基，苯基或苯基-C 1-3烷基，该苯基部分可被C 1-6烷基，C 1-6烷氧基，CF 3或卤素取代; R 5和R 6中的另一个是氢或C 1-6烷基; （II）其中R 2，R 3和R 4各自独立地选自氢，卤素，CF 3 + L，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，C 1 -7酰基，C 1-7羧基酰基氨基，C 1-6烷基磺酰基氨基，N-（C 1-6烷基磺酰基）-N-C 1-4烷基氨基，C 1-6烷基磺酰基，C 1-6烷基亚磺酰基，羟基，硝基或氨基，氨基羰基，氨基磺酰基 ，氨基磺酰基氨基或N-（氨基磺酰基）-C 1-4烷基氨基，其任选地被选自C 1-6烷基，C 3-8环烷基，C 3-8环烷基C 1-4烷基，苯基或苯基C 1-4烷基中的一个或两个基团N-取代 基团或任选被C4-5多亚甲基N-二取代; 或两者一起是C1-2亚烷基二氧基; （i）R 1独立地是除氢以外的R 2，R 3或R 4的任何一个或与R 2一起为C1-2亚烷基二氧基，C1-2氧化烯硫代，C2-3亚烷基氧基或N-（C1-2氧亚烷基）-N- C 1-6烷基氨基; X和Y之一是CO，另一个是NH; 或（ii）X为CO且Y为NR16，其中R 1和R 16一起为C 1-2亚烷基; 式（I）中描述的氮原子与部分A中最近的氮原子分开至少2个碳原子; 其制法及其组合物。

公开(公告)号：US4607033A

公开(公告)日：1986-08-19

申请号：US666818

申请日：1984-10-31

申请人： Barrie C. C. Cantello

发明人： Barrie C. C. Cantello

IPC分类号： A61K31/535 ,  A61K31/5375 ,  A61K31/55 ,  A61P3/04 ,  A61P3/08 ,  C07D265/30 ,  C07D267/08 ,  C07D267/10 ,  C07D413/04

CPC分类号： C07D265/30 ,  C07D267/10 ,  C07D413/04

摘要： Compounds of formula (I): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group,R.sup.1 is hydrogen or methyl,R.sup.2 is carboxyl or a group O--Z--CO.sub.2 H or an ester or amide thereof; a groupO--E--NR.sup.3 R.sup.4 or a group O--E--OR.sup.5,wherein R.sup.3, R.sup.4 and R.sup.5 each represents hydrogen or C.sub.1-6 alkyl, Z is a C.sub.1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2 ; a process for the production of such compounds and their use in treating hyperglycaemia and/or obesity.

摘要翻译： 式（I）化合物：其中W为任选被卤素或三氟甲基取代的苯基或苯并呋喃-2-基，R1为氢或甲基，R2为羧基或 基团OZ-CO 2 H或其酯或酰胺; 基团OE-NR3R4或OE-OR5基团，其中R3，R4和R5各自表示氢或C1-6烷基，Z是C1-6直链或支链亚烷基链，n是1或2，a是2或3 并且E是具有至少两个碳原子的C2-7直链或支链亚烷基链，其分离基团R2中的两个杂原子; 这种化合物的制备方法及其在治疗高血糖症和/或肥胖症中的用途。

公开(公告)号：US4596800A

公开(公告)日：1986-06-24

申请号：US756795

申请日：1985-07-19

申请人： Anthony T. Ainsworth ,  Richard M. Hindley

发明人： Anthony T. Ainsworth ,  Richard M. Hindley

IPC分类号： A61K31/535 ,  A61K31/5375 ,  A61K31/538 ,  A61P3/08 ,  C07C67/00 ,  C07C213/00 ,  C07C225/16 ,  C07C227/00 ,  C07C227/08 ,  C07C229/22 ,  C07C231/00 ,  C07C231/12 ,  C07C235/06 ,  C07C235/20 ,  C07C237/06 ,  C07D265/32 ,  C07D265/36 ,  C07D265/30

CPC分类号： C07D265/32 ,  C07D265/36

摘要： A compound of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl;R.sup.2 is hydrogen or halogen;R.sup.3 is hydrogen or methyl;R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H or an ester or amide derivative thereof, O(CH.sub.2).sub.b M or --CO.sub.2 H or an ester or amide derivative thereofwhereina is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring; R.sup.5 is C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted by carboxy or esters and amides thereof; or phenyl optionally substituted by C.sub.1-6 alkyl, halogen, alkoxy or trifluoromethyl;R.sup.8 is hydrogen or C.sub.1-6 alkyl or R.sup.8 together withR.sup.5 form a carbocyclic ring; andn is 1 or 2.Processes for preparing these compounds and their use in therapy is also described.

摘要翻译： 式（I）化合物其中R 1是氢，卤素或三氟甲基;或其药学上可接受的盐，其中R 1是氢，卤素或三氟甲基; R2是氢或卤素; R3是氢或甲基; R 4是-O（CH 2）a CO 2 H或其酯或酰胺衍生物，O（CH 2）b M或-CO 2 H或其酯或酰胺衍生物，其中a是1至6的整数，b是2至7的整数 ，和M是羟基，C 1-6烷氧基或者其中R 6和R 7各自是氢或C 1-6烷基或者一起形成五或六元环; R5是C1-6烷基; 被羧基或其酯和酰胺取代的C 1-6烷基; 或任选被C 1-6烷基，卤素，烷氧基或三氟甲基取代的苯基; R8是氢或C1-6烷基或R8与R5一起形成碳环; 并且n为1或2.还描述了制备这些化合物及其在治疗中的用途的方法。